ES2162933T3 - USEFUL COMPOUNDS AS ANTIPROLIFERATIVE AND INHIBITING AGENTS OF THE RIBONUCLEOTIDO GLIBINAMIDE FORMULO TRANSFERASA (GARFT) ENZYME - Google Patents

USEFUL COMPOUNDS AS ANTIPROLIFERATIVE AND INHIBITING AGENTS OF THE RIBONUCLEOTIDO GLIBINAMIDE FORMULO TRANSFERASA (GARFT) ENZYME

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Publication number
ES2162933T3
ES2162933T3 ES95927503T ES95927503T ES2162933T3 ES 2162933 T3 ES2162933 T3 ES 2162933T3 ES 95927503 T ES95927503 T ES 95927503T ES 95927503 T ES95927503 T ES 95927503T ES 2162933 T3 ES2162933 T3 ES 2162933T3
Authority
ES
Spain
Prior art keywords
sub
instituted
group
replaced
substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES95927503T
Other languages
Spanish (es)
Inventor
Michael D Varney
William H Romines
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Agouron Pharmaceuticals LLC
Original Assignee
Agouron Pharmaceuticals LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Agouron Pharmaceuticals LLC filed Critical Agouron Pharmaceuticals LLC
Application granted granted Critical
Publication of ES2162933T3 publication Critical patent/ES2162933T3/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Abstract

COMPUESTOS DE FORMULA (I), LOS CUALES ESTAN EN EQUILIBRIO CON SUS TAUTOMEROS 4-HIDROXI Y ESTAN EN FORMA DE MEZCLAS DIAESTEREOMERICAS, Y SUS SALES FARMACEUTICAMENTE ACEPTABLES SON POTENTES INHIBIDORES DE GARFT. A ES S, CH{SUB,2} O SE; Z ES UN ALQUILO C{SUB,1}-C{SUB,3} SUSTITUIDO O INSUSTITUIDO, ALQUENILO C{SUB,2}-C{SUB,3}, ALQUINILO C{SUB,2}-C{SUB,3} O GRUPO AMINO, O S O O; X ES UN GRUPO ALQUILO C{SUB,1}-C{SUB,6} SUSTITUIDO O INSUSTITUIDO; UN GRUPO ALQUINILO C{SUB,2}-C{SUB,6} SUSTITUIDO O INSUSTITUIDO; UN GRUPO ALQUINILO C{SUB,2}-C{SUB,6} SUSTITUIDO O INSUSTITUIDO; -C(()O())E, EN DONDE E ES HIDROGENO, UN GRUPO ALQUILO C{SUB,1}-C{SUB,3} SUSTITUIDO O INSUSTITUIDO, UN GRUPO ALQUENILO C{SUB,2}-C{SUB,3} SUSTITUIDO O INSUSTITUIDO, UN GRUPO ALQUINILO C{SUB,2}-C{SUB,3} SUSTITUIDO O INSUSTITUIDO, UN GRUPO ALCOXI OC{SUB,1}-C{SUB,3} SUSTITUIDO O INSUSTITUIDO, O NR{SUB,10}R{SUB,11}, EN DONDE R{SUB,10} Y R{SUB,11} SE SELECCIONAN INDEPENDIENTEMENTE DE HIDROGENO, GRUPOS ALQUILO C{SUB,1}-C{SUB,3} SUSTITUIDOS E INSUSTITUIDOS, GRUPOS ALQUENILO C{SUB,2}-C{SUB,3} SUSTITUIDOS E INSUSTITUIDOS, GRUPOS ALQUINILO C{SUB,2}-C{SUB,3} SUSTITUIDOS E INSUSTITUIDOS; NR{SUB,10}R{SUB,11}, EN DONDE R{SUB,10} Y R{SUB,11} SE DEFINEN INDEPENDIENTEMENTE COMO SE ESTABLECE ANTES; HIDROXILO, NITRO; SR{SUB,12} EN DONDE R{SUB,12} ES HIDROGENO, UN GRUPO ALQUILO C{SUB,1}-C{SUB,6} SUSTITUIDO O INSUSTITUIDO, UN GRUPO ALQUENILO C{SUB,2}-C{SUB,6} SUSTITUIDO O INSUSTITUIDO O UN GRUPO ALQUINILO C{SUB,2}-C{SUB,6} SUSTITUIDO O INSUSTITUIDO; CIANO; O UN GRUPO ALCOXI C{SUB,1}-C{SUB,3} SUSTITUIDO O INSUSTITUIDO; Y R{SUB,1} Y R{SUB,2} SON INDEPENDIENTEMENTE HIDROGENO O UNA ESTRUCTURA QUE FORMA CON EL CO{SUB,2} INCORPORADO UN GRUPO DE ESTER RAPIDAMENTE HIDROLIZABLE. ESTOS COMPUESTOS Y SUS SALES SON UTILES COMO AGENTES ANTIPROLIFERATIVOS. LA INVENCION TAMBIEN PERTENECE A COMPOSICIONES FARMACEUTICAS Y A METODOS QUE EMPLEAN DICHOS COMPUESTOS COMO AGENTES INHIBIDORES O ANTIPROLIFERATIVOS DE GARFT. LA INVENCION TAMBIEN SE REFIERE A COMPUESTOS UTILES COMO INTERMEDIARIOS PARA LA PREPARACION DE DICHOS COMPUESTOS, Y A SUS SINTESIS.FORMULA COMPOUNDS (I), WHICH ARE IN BALANCE WITH ITS 4-HYDROXI TAUTOMERS AND ARE IN THE FORM OF DIAESTEREOMERIC MIXTURES, AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS ARE POWERFUL GARBAL INHIBITORS. A ES S, CH {SUB, 2} OR SE; Z IS A RENT C {SUB, 1} -C {SUB, 3} REPLACED OR INSTITUTED, RENT C {SUB, 2} -C {SUB, 3}, RENT C {SUB, 2} -C {SUB, 3} OR AMINO GROUP, OSOO; X IS A C {SUB, 1} -C {SUB, 6} RENTED GROUP REPLACED OR INSTITUTED; AN ALQUINILO GROUP C {SUB, 2} -C {SUB, 6} REPLACED OR INSTITUTED; AN ALQUINILO GROUP C {SUB, 2} -C {SUB, 6} REPLACED OR INSTITUTED; -C (() O ()) E, WHERE E IS HYDROGEN, A RENTING GROUP C {SUB, 1} -C {SUB, 3} REPLACED OR INSTITUTED, A RENTING GROUP C {SUB, 2} -C {SUB , 3} REPLACED OR INSTITUTED, AN ALQUINYL GROUP C {SUB, 2} -C {SUB, 3} REPLACED OR INSTITUTED, AN ALCOXI GROUP OC {SUB, 1} -C {SUB, 3} REPLACED OR INSTITUTED, OR NR { SUB, 10} R {SUB, 11}, WHERE R {SUB, 10} YR {SUB, 11} ARE SELECTED INDEPENDENTLY FROM HYDROGEN, GROUPS FOR RENT C {SUB, 1} -C {SUB, 3} SUBSTITUTED AND INSTITUTED, GROUPS ALQUENILO C {SUB, 2} -C {SUB, 3} SUBSTITUTED AND INSTITUTED, GROUPS ALQUINILO C {SUB, 2} -C {SUB, 3} SUBSTITUTED AND INSTITUTED; NR {SUB, 10} R {SUB, 11}, WHERE R {SUB, 10} AND R {SUB, 11} ARE DEFINED INDEPENDENTLY AS SET BEFORE; HYDROXYL, NITRO; SR {SUB, 12} WHERE R {SUB, 12} IS HYDROGEN, A RENTING GROUP C {SUB, 1} -C {SUB, 6} REPLACED OR INSTITUTED, A RENTING GROUP C {SUB, 2} -C {SUB , 6} SUBSTITUTED OR INSTITUTED OR AN ALQUINYL GROUP C {SUB, 2} -C {SUB, 6} REPLACED OR INSTITUTED; Cyan; OR AN ALCOXI GROUP C {SUB, 1} -C {SUB, 3} SUBSTITUTED OR INSTITUTED; AND R {SUB, 1} AND R {SUB, 2} ARE INDEPENDENTLY HYDROGEN OR A STRUCTURE FORMING WITH THE CO {SUB, 2} INCORPORATED A RAPIDLY HYDROLIZABLE ESTER GROUP. THESE COMPOUNDS AND THEIR SALTS ARE USEFUL AS ANTIPROLIFERATIVE AGENTS. THE INVENTION ALSO BELONGS TO PHARMACEUTICAL COMPOSITIONS AND METHODS THAT USE THOSE COMPOUNDS AS INHIBITING OR ANTIPROLIFERATIVE AGENTS OF GARFT. THE INVENTION ALSO REFERS TO USEFUL COMPOUNDS AS INTERMEDIARIES FOR THE PREPARATION OF SUCH COMPOUNDS, AND THEIR SYNTHESIS.

ES95927503T 1994-07-28 1995-07-28 USEFUL COMPOUNDS AS ANTIPROLIFERATIVE AND INHIBITING AGENTS OF THE RIBONUCLEOTIDO GLIBINAMIDE FORMULO TRANSFERASA (GARFT) ENZYME Expired - Lifetime ES2162933T3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/281,639 US5608082A (en) 1994-07-28 1994-07-28 Compounds useful as antiproliferative agents and GARFT inhibitors

Publications (1)

Publication Number Publication Date
ES2162933T3 true ES2162933T3 (en) 2002-01-16

Family

ID=23078167

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95927503T Expired - Lifetime ES2162933T3 (en) 1994-07-28 1995-07-28 USEFUL COMPOUNDS AS ANTIPROLIFERATIVE AND INHIBITING AGENTS OF THE RIBONUCLEOTIDO GLIBINAMIDE FORMULO TRANSFERASA (GARFT) ENZYME

Country Status (20)

Country Link
US (2) US5608082A (en)
EP (1) EP0773943B1 (en)
JP (1) JPH10503762A (en)
KR (1) KR100380610B1 (en)
CN (2) CN1091770C (en)
AT (1) ATE206122T1 (en)
AU (1) AU697138B2 (en)
CA (1) CA2195420A1 (en)
DE (1) DE69522945T2 (en)
DK (1) DK0773943T3 (en)
ES (1) ES2162933T3 (en)
FI (1) FI112079B (en)
MX (1) MX9700675A (en)
NO (1) NO308248B1 (en)
NZ (1) NZ290703A (en)
PT (1) PT773943E (en)
RU (1) RU2152945C2 (en)
SI (1) SI0773943T1 (en)
TW (1) TW432062B (en)
WO (1) WO1996003406A1 (en)

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US20040006077A1 (en) * 2002-06-25 2004-01-08 Bernard Gaudilliere Thiazine and oxazine derivatives as MMP-13 inhibitors
CA2489722A1 (en) * 2002-07-17 2004-01-22 William Howard Roark Combination of an allosteric alkyne inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
WO2004113337A1 (en) * 2003-06-25 2004-12-29 Pfizer Inc. Convergent synthesis of a garft inhibitor containing a methyl substitute thiophene core and a tetrahydropyrido`2,3-d! pyrimidine ring system and intermediates therefor
WO2004113328A1 (en) * 2003-06-25 2004-12-29 Pfizer Inc. Convergent asymmetric synthesis route to produce a key intermediate towards the synthesis of a garft inhibitor
WO2005016926A1 (en) * 2003-08-19 2005-02-24 Warner-Lambert Company Llc Pyrido [3,4-d] pyrimidine derivatives as matrix metalloproteinase-13 inhibitors
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Also Published As

Publication number Publication date
MX9700675A (en) 1997-04-30
NO970349L (en) 1997-03-12
CA2195420A1 (en) 1996-02-08
ATE206122T1 (en) 2001-10-15
AU3151795A (en) 1996-02-22
CN1091770C (en) 2002-10-02
JPH10503762A (en) 1998-04-07
US5646141A (en) 1997-07-08
RU2152945C2 (en) 2000-07-20
NO308248B1 (en) 2000-08-21
TW432062B (en) 2001-05-01
FI970317A0 (en) 1997-01-24
FI112079B (en) 2003-10-31
KR100380610B1 (en) 2003-08-27
PT773943E (en) 2002-01-30
EP0773943B1 (en) 2001-09-26
AU697138B2 (en) 1998-09-24
FI970317A (en) 1997-03-05
CN1394857A (en) 2003-02-05
DK0773943T3 (en) 2002-03-04
SI0773943T1 (en) 2001-12-31
US5608082A (en) 1997-03-04
NZ290703A (en) 1998-11-25
CN1154110A (en) 1997-07-09
DE69522945T2 (en) 2002-03-28
EP0773943A1 (en) 1997-05-21
WO1996003406A1 (en) 1996-02-08
NO970349D0 (en) 1997-01-27
DE69522945D1 (en) 2001-10-31

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